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Brigatinib C

Cat. No. M43427
Brigatinib C Structure
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Biological Activity

Brigatinib C is a linker, as a part of PROTAC Linker to target HJM-561.

Chemical Information
Molecular Weight 570.07
Formula C28H37ClN7O2P
CAS Number 1197958-75-0
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Aditya Shreenivas et al. NPJ Precis Oncol. ALK fusions in the pan-cancer setting: another tumor-agnostic target?

[2] Antonia A Högnäsbacka et al. J Med Chem. Synthesis and Preclinical Evaluation of [ Methylpiperazine-11C]brigatinib as a PET Tracer Targeting Both Mutated Epidermal Growth Factor Receptor and Anaplastic Lymphoma Kinase

[3] Michael J Hanley et al. Invest New Drugs. Brigatinib pharmacokinetics in patients with chronic hepatic impairment

[4] Sheridan M Hoy. Drugs. Brigatinib: A Review in ALK-Inhibitor Naïve Advanced ALK-Positive NSCLC

[5] D Ross Camidge et al. N Engl J Med. Brigatinib versus Crizotinib in ALK-Positive Non-Small-Cell Lung Cancer

Related PROTAC Linker Products
m-PEG-OH(MW5000)

m-PEG-OH is a PROTAC linker and belongs to the PEG class. It can be used to synthesize PROTAC molecules.

tert-butyl 4-(3,3-difluoropiperidin-4-yl)piperazine-1-carboxylate

tert-butyl 4-(3,3-difluoropiperidin-4-yl)piperazine-1-carboxylate is a PROTAC linker that can be used in the synthesis of PROTACs.

Tert-butyl 4-((1-((benzyloxy)carbonyl)piperidin-4-yl)methyl)piperazine-1-carboxylate

Tert-butyl 4-((1-((benzyloxy)carbonyl)piperidin-4-yl)methyl)piperazine-1-carboxylate is a PROTAC linker that can be used in the synthesis of PROTACs.

Tert-butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate

Tert-butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate is a PROTAC linker that can be used in the synthesis of PROTACs.

Lenalidomide-acetylene-Br

Lenalidomide-acetylene-Br is a PROTAC Linker taht makes up HJM-561.

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Keywords: Brigatinib C supplier, PROTAC Linker, inhibitors, activators


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